EP2682387A3 - C7-fluoro substituted tetracycline compounds - Google Patents

C7-fluoro substituted tetracycline compounds Download PDF

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Publication number
EP2682387A3
EP2682387A3 EP20130172357 EP13172357A EP2682387A3 EP 2682387 A3 EP2682387 A3 EP 2682387A3 EP 20130172357 EP20130172357 EP 20130172357 EP 13172357 A EP13172357 A EP 13172357A EP 2682387 A3 EP2682387 A3 EP 2682387A3
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EP
European Patent Office
Prior art keywords
fluoro substituted
tetracycline compounds
substituted tetracycline
structural formula
compound
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP20130172357
Other languages
German (de)
French (fr)
Other versions
EP2682387B1 (en
EP2682387A2 (en
Inventor
Robert B. Zahler
Roger B. Clark
Diana Katharine Hunt
Louis Plamondon
Xiao-Yi Xiao
Jingye Zhou
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Tetraphase Pharmaceuticals Inc
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Tetraphase Pharmaceuticals Inc
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Priority to SI200931338T priority Critical patent/SI2682387T1/en
Priority to PL13172357T priority patent/PL2682387T3/en
Priority to EP15180611.4A priority patent/EP3000805B1/en
Priority to PL15180611T priority patent/PL3000805T3/en
Application filed by Tetraphase Pharmaceuticals Inc filed Critical Tetraphase Pharmaceuticals Inc
Publication of EP2682387A2 publication Critical patent/EP2682387A2/en
Publication of EP2682387A3 publication Critical patent/EP2682387A3/en
Publication of EP2682387B1 publication Critical patent/EP2682387B1/en
Application granted granted Critical
Priority to HRP20151368TT priority patent/HRP20151368T1/en
Priority to CY20151101188T priority patent/CY1117085T1/en
Active legal-status Critical Current
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/57Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/65Tetracyclines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
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    • C07C237/26Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton of a ring being part of a condensed ring system formed by at least four rings, e.g. tetracycline
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    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

The present invention is directed to a compound falling under Structural Formula (A): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.
EP13172357.9A 2008-08-08 2009-08-07 C7-fluoro substituted tetracycline compounds Active EP2682387B1 (en)

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SI200931338T SI2682387T1 (en) 2008-08-08 2009-08-07 C7-fluoro substituted tetracycline compounds
PL13172357T PL2682387T3 (en) 2008-08-08 2009-08-07 C7-fluoro substituted tetracycline compounds
EP15180611.4A EP3000805B1 (en) 2008-08-08 2009-08-07 C7-fluoro substituted tetracycline compounds
PL15180611T PL3000805T3 (en) 2008-08-08 2009-08-07 C7-fluoro substituted tetracycline compounds
HRP20151368TT HRP20151368T1 (en) 2008-08-08 2015-12-11 C7-fluoro substituted tetracycline compounds
CY20151101188T CY1117085T1 (en) 2008-08-08 2015-12-23 C7-Fluorine Substituted Tetracycline Compounds

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Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2009279473B2 (en) 2008-08-08 2012-12-13 Tetraphase Pharmaceuticals, Inc. C7-fluoro substituted tetracycline compounds
CA2761241C (en) 2009-05-08 2018-02-27 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds
CN105622496B (en) 2009-08-28 2019-03-05 四相制药公司 Tetracycline compound
WO2012021829A1 (en) * 2010-08-12 2012-02-16 Tetraphase Pharmaceuticals, Inc. Methods of treating bacterial infections
AR082633A1 (en) * 2010-08-12 2012-12-19 Tetraphase Pharmaceuticals Inc TETRACICLINE ANALOGS
WO2012065028A2 (en) 2010-11-11 2012-05-18 Concert Pharmaceuticals Inc. Substituted tetracyclines
EP2890673B1 (en) 2012-08-31 2018-11-14 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds
CN104230960B (en) * 2013-06-06 2017-02-15 山东轩竹医药科技有限公司 Four-ring anaplastic lymphoma kinase inhibitor
MA40836A (en) 2014-10-23 2017-08-29 Tetraphase Pharmaceuticals Inc SEMI-SYNTHESIS PROCEDURES
WO2017097891A1 (en) 2015-12-10 2017-06-15 Sandoz Ag Crystalline eravacycline
ES2834049T3 (en) 2016-01-22 2021-06-16 Sandoz Ag Crystalline Eravacycline Bischloride
AU2017259960A1 (en) * 2016-05-02 2018-12-06 Paratek Pharmaceuticals, Inc. 9-aminomethyl minocycline compounds and methods of use thereof in urinary tract infection (UTI) treatment
CN107759503A (en) * 2016-08-16 2018-03-06 四川科伦博泰生物医药股份有限公司 A kind of tetracycline derivant and application thereof
SG10202101986UA (en) 2016-08-30 2021-04-29 Tetraphase Pharmaceuticals Inc Tetracycline compounds and methods of treatment
MA46567A (en) 2016-10-19 2019-08-28 Tetraphase Pharmaceuticals Inc ERAVACYCLINE CRYSTALLINE FORMS
CN110087655A (en) 2016-11-01 2019-08-02 帕拉特克药品公司 9- Aminomethyl Minocycline compound and its purposes in treatment Community-acquired bacterial pneumonia (CABP)
WO2020097450A1 (en) 2018-11-09 2020-05-14 Tetraphase Pharmaceuticals, Inc. Polymorphic forms of a compound and uses thereof
WO2023233397A1 (en) * 2022-05-29 2023-12-07 B. G. Negev Technologies And Applications Ltd., At Ben-Gurion University Eravacycline for treating cancer

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB935384A (en) * 1959-03-30 1963-08-28 Pfizer & Co C Tetracycline derivatives and preparation thereof
EP0582789A1 (en) * 1992-08-13 1994-02-16 American Cyanamid Company Novel 7-(substituted)-8-(substituted)-9- (substituted glycyl)amido -6-demethyl-6-deoxytetracyclines

Family Cites Families (80)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3338963A (en) * 1960-10-28 1967-08-29 American Cyanamid Co Tetracycline compounds
GB1034933A (en) 1962-10-29 1966-07-06 American Cyanamid Co 4-demethylamino-4-substituted amino 6-demethyl tetracyclines
US3304227A (en) 1965-07-15 1967-02-14 Loyal E Loveless Antibiotic-containing animal feed
US3433709A (en) * 1965-12-07 1969-03-18 American Cyanamid Co Biological transformation of alpha-6-deoxytetracyclines to tetracyclines
US4935412A (en) 1983-12-29 1990-06-19 The Research Foundation Of State University Of New York Non-antibacterial tetracycline compositions possessing anti-collagenolytic properties and methods of preparing and using same
US4704383A (en) 1983-12-29 1987-11-03 The Research Foundation Of State University Of New York Non-antibacterial tetracycline compositions possessing anti-collagenolytic properties and methods of preparing and using same
US4666897A (en) 1983-12-29 1987-05-19 Research Foundation Of State University Inhibition of mammalian collagenolytic enzymes by tetracyclines
USRE34656E (en) 1983-12-29 1994-07-05 The Research Foundation Of State University Of New York Use of tetracycline to enhance bone protein synthesis and/or treatment of bone deficiency
US4925833A (en) 1983-12-29 1990-05-15 The Research Foundation Of State University Of New York Use of tetracycline to enhance bone protein synthesis and/or treatment of osteoporosis
JP3016587B2 (en) 1989-12-04 2000-03-06 ザ・リサーチ・ファンデーション・オブ・ステート・ユニバーシティ・オブ・ニューヨーク Combination of non-steroidal anti-inflammatory drug and tetracycline
US5308839A (en) 1989-12-04 1994-05-03 The Research Foundation Of State University Of New York Composition comprising non-steroidal anti-inflammatory agent tenidap and effectively non-antibacterial tetracycline
US5770588A (en) 1991-02-11 1998-06-23 The Research Foundation Of State University Of New York Non-antibacterial tetracycline compositions of the prevention and treatment of root caries
US5231017A (en) 1991-05-17 1993-07-27 Solvay Enzymes, Inc. Process for producing ethanol
USRE40183E1 (en) 1991-10-04 2008-03-25 Wyeth Holdings Corporation 7-Substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines
DE69232302D1 (en) * 1991-10-04 2002-01-31 American Cyanamid Co 7-Substituted-9-substituted amino-6-demethyl-6-deoxy-tetracyclines
US5494903A (en) 1991-10-04 1996-02-27 American Cyanamid Company 7-substituted-9-substituted amino-6-demethyl-6-deoxytetracyclines
US5258371A (en) 1992-05-29 1993-11-02 Kuraray Co., Ltd. Method to reduce connective tissue destruction
US6043225A (en) 1992-06-12 2000-03-28 Board Of Regents Of The University Of Washington Diagnosis and treatment of arterial chlamydial granuloma
US5284963A (en) 1992-08-13 1994-02-08 American Cyanamid Company Method of producing 7-(substituted)-9-[(substituted glycyl)-amidol]-6-demethyl-6-deoxytetra-cyclines
SG47520A1 (en) 1992-08-13 1998-04-17 American Cyanamid Co New method for the production of 9-amino-6-demethyl-6-deoxytetracycline
US5328902A (en) 1992-08-13 1994-07-12 American Cyanamid Co. 7-(substituted)-9-[(substituted glycyl)amido]-6-demethyl-6-deoxytetracyclines
EP0599397B1 (en) 1992-11-17 1996-08-28 The Research Foundation Of State University Of New York Tetracyclines including non-antimicrobial chemically-modified tetracyclines inhibit excessive collagen crosslinking during diabetes
US5523297A (en) 1993-03-02 1996-06-04 The Research Foundation Of State University Of New York Inhibition of excessive phospholipase A2 activity and/or production by non-antimicrobial tetracyclines
US6043231A (en) 1993-03-02 2000-03-28 The Research Foundation Of State Univ. Of New York Inhibition of excessive phospholipase A2 activity and/or production by non-antimicrobial tetracyclines
US5371076A (en) * 1993-04-02 1994-12-06 American Cyanamid Company 9-[(substituted glycyl)amido]-6-(substituted)-5-hydroxy-6-deoxytetracyclines
US5668122A (en) 1993-07-28 1997-09-16 Fife; Rose S. Method to treat cancer with tetracyclines
US5834450A (en) 1994-02-17 1998-11-10 Pfizer Inc. 9- (substituted amino) -alpha-6-deoxy-5-oxy tetracycline derivatives, their preparation and their use as antibiotics
US5574026A (en) * 1994-12-13 1996-11-12 American Cyanamid Company Methods for inhibiting angiogenesis proliferation of endothelial or tumor cells and tumor growth
US5843925A (en) 1994-12-13 1998-12-01 American Cyanamid Company Methods for inhibiting angiogenesis, proliferation of endothelial or tumor cells and tumor growth
US5495301A (en) * 1994-12-27 1996-02-27 Zenith Electronics Corporation Three wire pillow speaker with full television remote control functions
US5834449A (en) 1996-06-13 1998-11-10 The Research Foundation Of State University Of New York Treatment of aortic and vascular aneurysms with tetracycline compounds
US5827840A (en) 1996-08-01 1998-10-27 The Research Foundation Of State University Of New York Promotion of wound healing by chemically-modified tetracyclines
US5789395A (en) 1996-08-30 1998-08-04 The Research Foundation Of State University Of New York Method of using tetracycline compounds for inhibition of endogenous nitric oxide production
US5919774A (en) 1996-12-10 1999-07-06 Eli Lilly And Company Pyrroles as sPLA2 inhibitors
US5837696A (en) 1997-01-15 1998-11-17 The Research Foundation Of State University Of New York Method of inhibiting cancer growth
US5773430A (en) 1997-03-13 1998-06-30 Research Foundation Of State University Of New York Serine proteinase inhibitory activity by hydrophobic tetracycline
US5929055A (en) 1997-06-23 1999-07-27 The Research Foundation Of State University Of New York Therapeutic method for management of diabetes mellitus
US6277061B1 (en) 1998-03-31 2001-08-21 The Research Foundation Of State University Of New York Method of inhibiting membrane-type matrix metalloproteinase
US6015804A (en) 1998-09-11 2000-01-18 The Research Foundation Of State University Of New York Method of using tetracycline compounds to enhance interleukin-10 production
US5977091A (en) 1998-09-21 1999-11-02 The Research Foundation Of State University Of New York Method of preventing acute lung injury
US5998390A (en) 1998-09-28 1999-12-07 The Research Foundation Of State University Of New York Combination of bisphosphonate and tetracycline
AU759372B2 (en) 1998-09-28 2003-04-10 Research Foundation Of The State University Of New York, The A novel inhibitor of cataract formation
US6914057B1 (en) 1998-09-28 2005-07-05 The Research Foundation Of State University Of New York Inhibitor of cataract formation
US6231894B1 (en) 1999-10-21 2001-05-15 Duke University Treatments based on discovery that nitric oxide synthase is a paraquat diaphorase
AU2000257445A1 (en) 2000-06-16 2002-01-02 Trustees Of Tufts College 7-n-substituted phenyl tetracycline compounds
DE60144375D1 (en) 2000-07-07 2011-05-19 Trustees Of Tufts College Medford 7-, 8-, and 9-SUBSTITUTED TETRACYCLIN COMPOUNDS
IL153639A0 (en) * 2000-07-07 2003-07-06 Tufts College 9-substituted minocycline compounds
EP1381372A2 (en) 2001-03-14 2004-01-21 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds as synergistic antifungal agents
CA2457234A1 (en) 2001-03-14 2002-09-19 Mark L. Nelson Substituted tetracycline compounds as antifungal agents
EP2186793A1 (en) 2001-04-24 2010-05-19 Paratek Pharmaceuticals, Inc. Substituted Tetracycline Compounds
US8088820B2 (en) 2001-04-24 2012-01-03 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for the treatment of malaria
US20060194773A1 (en) 2001-07-13 2006-08-31 Paratek Pharmaceuticals, Inc. Tetracyline compounds having target therapeutic activities
EP2327409A1 (en) 2001-07-13 2011-06-01 Paratek Pharmaceuticals, Inc. Tetracycline compound having target therapeutic activities
EP2311451A1 (en) 2002-03-08 2011-04-20 Paratek Pharmaceuticals, Inc. Amino-methyl substituted tetracycline compounds
WO2003079984A2 (en) 2002-03-21 2003-10-02 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
AU2003261161B2 (en) 2002-07-12 2009-09-10 Paratek Pharmaceuticals, Inc 3, 10, and 12a substituted tetracycline compounds
WO2004038001A2 (en) 2002-10-24 2004-05-06 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for the treatment of malaria
WO2004038000A2 (en) 2002-10-24 2004-05-06 Paratek Pharmaceuticals, Inc. Methods of using substituted tetracycline compounds to modulate rna
AU2004259659B2 (en) 2003-07-09 2011-11-03 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
BR122018069604B1 (en) 2004-05-21 2021-07-20 President And Fellows Of Harvard College TETRACYCLINE COMPOUNDS AND ANALOGUES THEREOF, USE OF SUCH COMPOUNDS, PHARMACEUTICAL COMPOSITION, AS WELL AS SYNTHESIZATION AND PREPARATION METHODS OF SUCH COMPOUNDS
WO2006047671A2 (en) 2004-10-25 2006-05-04 Paratek Pharmaceuticals, Inc. 4-aminotetracyclines and methods of use thereof
EP1848685A1 (en) 2005-02-04 2007-10-31 Paratek Pharmaceuticals, Inc. 11a, 12-derivatives of tetracycline compounds
CN101119964A (en) * 2005-02-15 2008-02-06 惠氏公司 9-substituted tetracyclines
AU2006272698B2 (en) 2005-07-21 2012-11-01 Paratek Pharmaceuticals, Inc. 10-substituted tetracyclines and methods of use thereof
WO2007087416A2 (en) 2006-01-24 2007-08-02 Paratek Pharaceuticals, Inc. Methods of increasing oral bioavailability of tetracyclines
AU2007235279B2 (en) 2006-04-07 2012-12-06 President And Fellows Of Harvard College Synthesis of tetracyclines and analogues thereof
AU2007249696A1 (en) 2006-05-15 2007-11-22 Paratek Pharmaceuticals, Inc. Methods of regulating expression of genes or of gene products using substituted tetracycline compounds
WO2008045507A2 (en) 2006-10-11 2008-04-17 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds for treatment of bacillus anthracis infections
EP2479169B1 (en) 2006-10-11 2014-12-03 President and Fellows of Harvard College Synthesis of Enone Intermediate
AU2008239606A1 (en) 2007-04-12 2008-10-23 Paratek Pharmaceuticals, Inc. Methods for treating spinal muscular atrophy using tetracycline compounds
WO2009032326A1 (en) * 2007-09-07 2009-03-12 Dr. Reddy's Laboratories Ltd. New tetracycline derivatives as antiinfective agents
WO2009128913A1 (en) 2008-04-14 2009-10-22 Paratek Pharmaceuticals, Inc. Substituted tetracycline compounds
AU2009279473B2 (en) * 2008-08-08 2012-12-13 Tetraphase Pharmaceuticals, Inc. C7-fluoro substituted tetracycline compounds
US9073829B2 (en) 2009-04-30 2015-07-07 President And Fellows Of Harvard College Synthesis of tetracyclines and intermediates thereto
CA2761241C (en) 2009-05-08 2018-02-27 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds
US8367654B2 (en) 2009-05-08 2013-02-05 Tetraphase Pharmaceuticals, Inc. 8-AZA tetracycline compounds
CN105622496B (en) 2009-08-28 2019-03-05 四相制药公司 Tetracycline compound
AR082633A1 (en) 2010-08-12 2012-12-19 Tetraphase Pharmaceuticals Inc TETRACICLINE ANALOGS
WO2012047907A1 (en) 2010-10-04 2012-04-12 President And Fellows Of Harvard College Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto
EP2890673B1 (en) 2012-08-31 2018-11-14 Tetraphase Pharmaceuticals, Inc. Tetracycline compounds

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB935384A (en) * 1959-03-30 1963-08-28 Pfizer & Co C Tetracycline derivatives and preparation thereof
EP0582789A1 (en) * 1992-08-13 1994-02-16 American Cyanamid Company Novel 7-(substituted)-8-(substituted)-9- (substituted glycyl)amido -6-demethyl-6-deoxytetracyclines

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
SATO, F. ET AL: "Structure-activity relationship investigation of some new tetracyclines by electronic index methodology", LOS ALAMOS NATIONAL LABORATORY, PREPRINT ARCHIVE, QUANTITATIVE BIOLOGY 1-18, ARXIV:0708.2931V1 [Q-BIO.BM], 21 AUG 2007 CODEN: LANLCJ URL: HTTP://ARXIV.ORG/PS_CACHE/ARXIV/PDF/0708/0708.2931V1.PDF, 2007, XP002548287 *

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